Design, Synthesis, and Evaluation of 2-Diethanolamino-4,8-diheptamethyleneimino-2-(N-aminoethyl-N-ethanolamino)-6-(N,N-diethanolamino)pyrimido[5,4-d]pyrimidine-fluorescein Conjugate (8MDP-fluor), As a Novel Equilibrative Nucleoside Transporter Probe

2011 ◽  
Vol 22 (6) ◽  
pp. 1221-1227 ◽  
Author(s):  
Wenwei Lin ◽  
John K. Buolamwini
Keyword(s):  
Nucleoside Transporter ◽  
Design Synthesis ◽  
Equilibrative Nucleoside Transporter

Contribution of equilibrative nucleoside transporter (ENT) 2 to fluorouracil transport in rat placental trophoblast cells

2017 ◽  
Vol 32 (2) ◽  
pp. 151-156 ◽  
Author(s):  
Akinori Takagi ◽  
Tomohiro Nishimura ◽  
Tomoya Akashi ◽  
Masatoshi Tomi ◽  
Emi Nakashima
Keyword(s):  
Nucleoside Transporter ◽  
Trophoblast Cells ◽  
Equilibrative Nucleoside Transporter

Nucleoside Transporter-guided Cytarabine Conjugated Liposomes for Intracellular Methotrexate Delivery and Cooperative Choriocarcinoma Therapy

2021 ◽  
Author(s):  
Weidong Fei ◽  
Yunchun Zhao ◽  
Xiaodong Wu ◽  
Dongli Sun ◽  
Yao Yao ◽  
...  
Keyword(s):  
Targeted Delivery ◽  
Rational Design ◽  
High Efficiency ◽  
Nucleoside Transporter ◽  
Childbearing Age ◽  
Equilibrative Nucleoside Transporter ◽  
Choriocarcinoma Cells ◽  
Tumor Accumulation ◽  
Novel Strategy ◽  
Distribution Studies

Abstract The gestational trophoblastic tumor seriously endangers child productive needs and the health of women in childbearing age. Nanodrug-based therapy mediated by transporters provides novel strategy for the treatment of trophoblastic tumors. Focus on the overexpressed human equilibrative nucleoside transporter 1 (ENT1) on the membrane of choriocarcinoma cells (JEG-3), the cytarabine (Cy, a substrate of ENT1) grafted liposome (Cy-Lipo) was introduced for targeted delivery of methotrexate (Cy-Lipo@MTX) for choriocarcinoma therapy in this study. The ENT1 has high affinity for Cy-Lipo and can mediate the endocytosis of the designed nanovehicles into JEG-3 cells. The ENT1 protein maintains its transporting function through circulation and regeneration during endocytosis. Therefore, Cy-Lipo-based formulations achieved high tumor accumulation and retention in pharmacokinetic and distribution studies. More importantly, the designed Cy-lipid conjugation exhibited a synergistic therapeutic effect on choriocarcinoma. Finally, Cy-Lipo@MTX exerts an extremely powerful anti-choriocarcinoma effect with fewer side effects. This study suggests that the overexpressed ENT1 on choriocarcinoma cells holds a great potential to be a high-efficiency target for the rational design of active targeting nanotherapeutics.

scholarly journals The role of the equilibrative nucleoside transporter 1 on tissue and fetal distribution of ribavirin in the mouse

2016 ◽  
Vol 37 (6) ◽  
pp. 336-344 ◽  
Author(s):  
Christopher J. Endres ◽  
Aaron M. Moss ◽  
Kazuya Ishida ◽  
Rajgopal Govindarajan ◽  
Jashvant D. Unadkat
Keyword(s):  
Nucleoside Transporter ◽  
Equilibrative Nucleoside Transporter
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